1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
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ABSTRACT:
SUBMITTER: Demont EH
PROVIDER: S-EPMC4233354 | biostudies-literature | 2014 Nov
REPOSITORIES: biostudies-literature
Publications
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Demont Emmanuel H EH Bamborough Paul P Chung Chun-Wa CW Craggs Peter D PD Fallon David D Gordon Laurie J LJ Grandi Paola P Hobbs Clare I CI Hussain Jameed J Jones Emma J EJ Le Gall Armelle A Michon Anne-Marie AM Mitchell Darren J DJ Prinjha Rab K RK Roberts Andy D AD Sheppard Robert J RJ Watson Robert J RJ
ACS medicinal chemistry letters 20140910 11
The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structure-activity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain. ...[more]
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